Opioid antagonist compounds have been approved by the FDA for some time for the complete or partial reversal of opioid intoxication. For example, naloxone was approved by the FDA in 1971 and first marketed as Narcan® injection for the complete or partial reversal of opioid intoxication. It has subsequently become a multisource prescription generic drug available in two strengths, 0.4 mg/mL and 1.0 mg/mL.
At present, naloxone is utilized by emergency services personnel for reversal of suspected opioid overdose. Hospital emergency departments carry this medication for the same purpose. Naloxone is also indicated as a reversal agent when the effects of therapeutic use of opioids are no longer medically necessary.
According to the Centers for Disease Control and Prevention, in 2008, poisoning became the leading cause of injury death in the United States. Nearly 9 out of 10 poisoning deaths are caused by drugs. During the past three decades, drug poisoning deaths increased by six fold, from about 6,100 in 1980 to about 36,500 in 2008. Between 1999 and 2008, the number of drug poisoning deaths involving opioid analgesics more than tripled from about 4,000 to about 14,800. In 2008, opioid analgesics were involved in more than 40% of drug poisonings, whereas in 1999, opioid analgesics were involved in 25% of drug poisoning.
Due to the increasing need for opioid overdose reversal agents, there is a need in the art for new and alternate compositions. Although naloxone is generally effective for opioid reversal, as with any medication, there are people who do not react well to naloxone. An alternative medication would be useful. The instant disclosure seeks to address one or more of these unmet needs.